PE20040764A1 - INDAZOLE DERIVATIVES AS ANTAGONISTS OF CORTICOTROPIN RELEASE FACTOR (CRF) - Google Patents

INDAZOLE DERIVATIVES AS ANTAGONISTS OF CORTICOTROPIN RELEASE FACTOR (CRF)

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Publication number
PE20040764A1
PE20040764A1 PE2003001215A PE2003001215A PE20040764A1 PE 20040764 A1 PE20040764 A1 PE 20040764A1 PE 2003001215 A PE2003001215 A PE 2003001215A PE 2003001215 A PE2003001215 A PE 2003001215A PE 20040764 A1 PE20040764 A1 PE 20040764A1
Authority
PE
Peru
Prior art keywords
alkyl
indazole
alcoxy
nrarb
aryl
Prior art date
Application number
PE2003001215A
Other languages
Spanish (es)
Inventor
Richard Leo Cournoyer
Counde O'yang
David Garrett Loughhead
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20040764A1 publication Critical patent/PE20040764A1/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Abstract

SE REFIERE A DERIVADOS DE INDAZOL DE FORMULA I O II, EN DONDE R2 ES H, ALQUILO(C1-C6), CICLOALQUILO(C3-C6), (CICLOALQUIL(C3-C6)-ALQUILO(C1-C3), (ALQUIL(C1-C6))CARBONILO, ALQUILSULFONILO(C1-C6), ARILO O ARILALQUILO QUE ESTAN EVENTUALMENTE SUSTITUIDOS POR ALQUILO(C1-C6), HALOALQUILO, ALCOXI (C1-C6) Y HALOGENO; R3 ES ARILO O HETEROARILO, EVENTUALMENTE SUSTITUIDOS POR DE ALQUILO(C1-C6), ALCOXI(C1-C6), ALQUILTIO(C1-C6), ALQUILSULFONILO(C1-C6), ENTRE OTROS; R1 EN EL CASO DE LA FORMULA I, ES -NRaRb, -CRcRdRe, CO2Ra o C(O)NRaRb; EN EL CASO DE LA FORMULA II ES NRaRb, CrcRdRe, CO2Ra; O EN EL CASO DE LAS FORMULAS I O II ES H, CICLOALQUENILO, ARILO O HETEROARILOQUE ESTAN EVENTUALMENTE SUSTITUIDOS POR ALQUILO(C1-C6), ALCOXI(C1-C6), ALQUILTIO(C1-C6), ALQUILSULFONILO(C1-C6), HALOGENO, ENTRE OTROS; Ra Y Rb SON H, ALQUILO(C1-C9), HIDROXIALQUILO, (ALCOXI C1-C6)-ALQUILO, ENTRE OTROS; O JUNTOS CON EL N FORMAN UN ANILLO HETEROCICLILO O HETEROARILO. SON COMPUESTOS PREFERIDOS: EL CLORHIDRATO DEL 7-(2,4-DICLORO-FENIL)-2-METIL-3-(1-PROPIL-BUT-1-ENIL)-2H-INDAZOL, CLORHIDRATO DE 2-METIL-3-(1-PROPIL-BUT-1-ENIL)-7-(2,4,6-TRIMETIL-FENIL)-2H-INDAZOL, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON ANTAGONISTAS DE RECEPTORES DEL FACTOR CRF Y PUEDEN USARSE PARA EL TRATAMIENTO DE TRANSTORNOS SIQUIATRICOS Y ENERMEDADES NEUROLOGICAS COMO LAS RELACIONADAS CON EL ESTRES, TRASTORNOS DE ANIMO, DE ALIMENTACION, DE ANSIEDAD, DISFUNCIONES GASTROINTESTINALES INDUCIDAS POR ESTRESREFERS TO INDAZOLE DERIVATIVES OF FORMULA IO II, WHERE R2 IS H, ALKYL (C1-C6), CYCLOALKYL (C3-C6), (CYCLOALKYL (C3-C6) -ALKYL (C1-C3), (ALKYL (C1 -C6)) CARBONYL, ALKYLSULPHONYL (C1-C6), ARYL OR ARYLALKYL WHICH ARE EVENTUALLY REPLACED BY ALKYL (C1-C6), HALOALKYL, ALCOXY (C1-C6) AND HALOGEN; EVENTUALLY IS ARYL OR HALOGENE ALKYL, EVENTUALLY SUBSTITUTED BY ALKYL (C1-C6), ALCOXY (C1-C6), ALKYLTIO (C1-C6), ALKYLSULFONILO (C1-C6), AMONG OTHERS; R1 IN THE CASE OF FORMULA I, IS -NRaRb, -CRcRdRe, CO2Ra or C ( O) NRaRb; IN THE CASE OF FORMULA II IT IS NRaRb, CrcRdRe, CO2Ra; OR IN THE CASE OF FORMULAS I OR II IT IS H, CYCLOALKENYL, ARYL OR HETEROARYL, WHICH ARE EVENTUALLY REPLACED BY ALKYL, (C1-C6) C6), ALKYLTIO (C1-C6), ALKYLSULFONYL (C1-C6), HALOGEN, AMONG OTHERS; Ra AND Rb ARE H, ALKYL (C1-C9), HYDROXYALKYL, (C1-C6 ALCOXY) -ALKYL, AMONG OTHERS; OR TOGETHER WITH N, THEY FORM A HETEROCYCLYL OR HETEROARYL RING.THE PREFERRED COMPOUNDS ARE: 7- (2,4-DICLO HYDROCHLORIDE RO-PHENYL) -2-METHYL-3- (1-PROPYL-BUT-1-ENYL) -2H-INDAZOLE, 2-METHYL-3- (1-PROPYL-BUT-1-ENYL) -7- ( 2,4,6-TRIMETHYL-PHENYL) -2H-INDAZOLE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. THESE COMPOUNDS ARE ANTAGONISTS OF RECEPTORS OF THE CRF FACTOR AND MAY BE USED FOR THE TREATMENT OF PSYCHIATRIC DISORDERS AND NEUROLOGICAL DISEASES SUCH AS THOSE RELATED TO STRESS, ANIMAL DISORDERS, EATING DISORDERS, ANXIETY, GASTROINTESTONE, DYSFUNCTION

PE2003001215A 2002-12-02 2003-11-28 INDAZOLE DERIVATIVES AS ANTAGONISTS OF CORTICOTROPIN RELEASE FACTOR (CRF) PE20040764A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US43016802P 2002-12-02 2002-12-02

Publications (1)

Publication Number Publication Date
PE20040764A1 true PE20040764A1 (en) 2004-11-06

Family

ID=32469420

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001215A PE20040764A1 (en) 2002-12-02 2003-11-28 INDAZOLE DERIVATIVES AS ANTAGONISTS OF CORTICOTROPIN RELEASE FACTOR (CRF)

Country Status (21)

Country Link
US (2) US7214699B2 (en)
EP (1) EP1569911B1 (en)
JP (1) JP4401298B2 (en)
KR (1) KR100761562B1 (en)
CN (1) CN100439341C (en)
AR (1) AR042148A1 (en)
AT (1) ATE399768T1 (en)
AU (1) AU2003286180B2 (en)
BR (1) BR0316950A (en)
CA (1) CA2507074A1 (en)
DE (1) DE60321958D1 (en)
ES (1) ES2309368T3 (en)
GT (1) GT200300263A (en)
MX (1) MXPA05005794A (en)
PA (1) PA8589601A1 (en)
PE (1) PE20040764A1 (en)
PL (1) PL377609A1 (en)
RU (1) RU2341518C2 (en)
TW (1) TW200418816A (en)
UY (1) UY28105A1 (en)
WO (1) WO2004050634A1 (en)

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AR065804A1 (en) 2007-03-23 2009-07-01 Smithkline Beecham Corp COMPOSITE OF INDOL CARBOXAMIDE, PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS IT AND USE OF THIS COMPOUND TO PREPARE A MEDICINAL PRODUCT
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Publication number Publication date
TW200418816A (en) 2004-10-01
GT200300263A (en) 2004-06-28
BR0316950A (en) 2006-01-17
KR20050084079A (en) 2005-08-26
US7214699B2 (en) 2007-05-08
RU2005120770A (en) 2006-02-10
KR100761562B1 (en) 2007-10-04
US20070213373A1 (en) 2007-09-13
JP4401298B2 (en) 2010-01-20
RU2341518C2 (en) 2008-12-20
WO2004050634A1 (en) 2004-06-17
ATE399768T1 (en) 2008-07-15
CN1732158A (en) 2006-02-08
EP1569911A1 (en) 2005-09-07
CA2507074A1 (en) 2004-06-17
AR042148A1 (en) 2005-06-08
JP2006510625A (en) 2006-03-30
MXPA05005794A (en) 2005-08-16
PA8589601A1 (en) 2004-09-16
AU2003286180A1 (en) 2004-06-23
PL377609A1 (en) 2006-02-06
ES2309368T3 (en) 2008-12-16
US20040110815A1 (en) 2004-06-10
DE60321958D1 (en) 2008-08-14
CN100439341C (en) 2008-12-03
AU2003286180B2 (en) 2009-11-12
EP1569911B1 (en) 2008-07-02
UY28105A1 (en) 2004-05-31

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